The thioesters are chemical substances formed by covalently bonding a sulfur atom to a acyl group, which is provided with a general formula as follows:

The thioesters are abundantly present in natural compounds, and are intermediate products during the hydrolysis or synthesis of ATP. The thioesters are required for forming all the ester bonds (including lipids). These substances are involved in the intracellular synthesis of a variety of materials, including peptides, fatty acids, steroids, terpenes, porphyrins, etc. The thioesters are also building blocks useful for organic synthesis and chemical synthesis of proteins. For example, the thioesters may be used to synthesize the thioesters with more complex structure, multi-substituted alkenes, thioethers, thiophene compounds and to react with amine compounds. The thioesters are also used as activated carboxylic acids and as acyl transfer agents for various nucleophiles.
Due to the unique structure of the thioesters, some thioesters possess biological activities and medicinal potential. For example, compound A as follows is an anti-inflammatory corticosteroid drug and compound B as follows may be used to treat Parkinson's disease.


Currently, the method in preparation of thioesters includes: (1) an esterification reaction between a carboxylic acid and a thiol; (2) a catalyzed transesterification reaction between a β-ketoester and a thiol; (3) a nucleophilic reaction between a cyclopropane derivative and a thiophenol; (4) carbonylation of allyl alcohol, propargyl alcohol, or diene and thiophenol; (5) carbonylation of a thioether. All of the methods mentioned above involve using a thiol, a thioether, or a thiophenol with a pungent smell.
In addition to the methods mentioned above, there is also a method for synthesizing of thioesters by using a thiourea instead of a thiol, a thioether, or a thiophenol with a pungent smell. The reaction scheme of the method is shown below. However, in addition to a thiourea, acyl halides, and organic halide, a surfactant and a base, such as K2CO3, NaOH, and the like, are further required for the method to obtain a thioester in higher yields.

Compared to the method mentioned above, the present invention provides a method for synthesizing of thioesters by a thiourea without a pungent smell, and free of activating agent.